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目的:通过体外实验,研究双环铂对人主动脉平滑肌细胞(HASMC)和人主动脉内皮细胞(HAEC)增殖的影响,探讨其成为支架携带药物的可能性。方法:3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲氧基胺)-2-(4-苯磺基)-2氢-四唑盐(MTS)法评价双环铂对HASMC和HAEC增殖的影响。探索不同浓度和不同作用时间条件下双环铂对HASMC和HAEC增殖抑制率的影响;双环铂对HASMC和HAEC半数抑制浓度的差异;以西罗莫斯作为阳性对照组,探索双环铂对HASMC和HAEC抗增殖作用的最低有效浓度。结果:双环铂对HASMC和HAEC的增殖抑制作用呈时间和浓度依赖性。双环铂对HASMC和HAEC的半数增殖抑制浓度分别为3.47μg/ml和72.44μg/ml。双环铂浓度为10 ng/ml～10μg/ml时,对HASMC有显著抑制作用(P<0.05)。双环铂浓度为10μg/ml时,对HAEC有显著抑制作用(P<0.01)。阳性对照药物西罗莫斯在纳克(ng)水平对HASMC和HAEC的增殖也有明显的抑制作用。结论:双环铂对HASMC和HAEC的增殖抑制作用呈时间和浓度依赖性。双环铂对HAEC的最低抑制浓度比对HASMC的最低抑制浓度高1000倍。尽管双环铂对细胞增殖的作用弱于西罗莫斯,但是其明显抑制血管平滑肌细胞增生而较少抑制血管内皮细胞增生的特性,使其有可能成为药物洗脱支架所携带的药物。
OBJECTIVE: To investigate the effects of bcl-2 on the proliferation of human aortic smooth muscle cells (HASMC) and human aortic endothelial cells (HAEC) in vitro and to explore its potential as a carrier for drugs. Method: 3- (4,5-Dimethylthiazol-2-yl) -5- (3- carboxymethoxyamine) -2- (4- Evaluation of Bicycloplatin on HASMC and HAEC Proliferation. To investigate the effects of Bcl-2 on the proliferation inhibition rate of HASMC and HAEC under different concentrations and different time periods; the difference of the half inhibitory concentration of Bcl-2 on HASMC and HAEC; and explore the inhibitory effect of Bcl-2 on HASMC and HAEC The least effective concentration of proliferation. RESULTS: Bcl-2 inhibited the proliferation of HASMC and HAEC in a time and concentration-dependent manner. The half inhibitory concentrations of Bcl-2 on HASMC and HAEC were 3.47μg / ml and 72.44μg / ml, respectively. When the concentration of bicycloplatin was 10 ng / ml ~ 10 μg / ml, HASMC was significantly inhibited (P <0.05). When the concentration of bicycloplatin was 10μg / ml, HAEC was significantly inhibited (P <0.01). The positive control drug, sirolimus, also had a significant inhibitory effect on the proliferation of HASMC and HAEC at the ng level. Conclusion: Bcl-2 inhibits the proliferation of HASMC and HAEC in a time and concentration-dependent manner. The minimum inhibitory concentration of bicyclo platinum to HAEC was 1000-fold higher than the lowest inhibitory concentration of HASMC. Although bicycloplatin is less effective than sirolimus on cell proliferation, its obvious inhibition of vascular smooth muscle cell proliferation with less inhibition of vascular endothelial cell proliferation makes it likely to be a drug carried by drug-eluting stents.